- Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors
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Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is a promising target for antimalarial chemotherapy and inhibition of this protease affects the growth of parasite adversely. A series of pyrido[1,2-a]pyrimidin-4-ones were synthesized and evaluat
- Mane,Li,Huang,Gupta,Nadkarni,Giridhar,Naik,Yadav
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p. 6296 - 6304
(2012/11/13)
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- Synthesis and characterisation of some new N-glycosides containing substituted pyridopyrimidinone, pyrimidopyridazinone, thiazolopyrimidinone and quinolizin-4-one moiety
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A series of new N-glycosides (D-glucosides, D-mannosides, L-and D-arabinosides, D-xylosides and one D-galactoside) containing heterocyclic moiety have been prepared by reaction of the corresponding heterocyclic amines with pyranoses in boiling methanol. The structures of the prepared compounds have been studied by means of proton and carbon NMR spectroscopy. In the most cases the products existed in DMSO solution as the single anomers. The Japan Institute of Heterocyclic Chemistry.
- Simunek, Petr,Svete, Jurij,Stanovnik, Branko
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experimental part
p. 2477 - 2491
(2011/04/17)
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- Methyl (Z)-2-[(benzyloxycarbonyl)amino]-3-dimethyl-aminopropenoate in the synthesis of heterocyclic systems. Synthesis of (benzyloxycarbonyl)amino substituted fused pyrimidinones
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Methyl (Z)-2-[(benzyloxycarbonyl)amino]-3-dimethylaminopropenoate (1) was used as a reagent for preparation of 3-[(benzyloxycarbonyl)amino] substituted 4H-pyrido[1,2-a]pyrimidin-4-ones 17-21, 4H-pyrimido[1,2-b]pyridazin-4-ones 22 and 23, 5H-[1,2,4]triazolo[2,3-a]-pyrimidin-5-one 24, 5H-thiazolo[3,2-a]pyrimidin-5-one 25, and 4H-pyrazino[1,2-a]pyrimidin-4-one 26. Removal of the benzyloxycarbonyl group by catalytical transfer hydrogenation with Pd/C in the presence of cyclohexene is selective to give 3-amino-4H-pyrido[1,2-a]-pyrimidin-4-ones 27-30 in 85-92% yields, or with hydrogen bromide in acetic acid to give 3-amino-4H-pyrimido[1,2-b]pyridazin-4-one (31) and 6-amino-5H-thiazolo[3,2-a]pyrimidin-5-one (32) in 80% yields.
- Toplak, Renata,Svete, Jurij,Golic Grdadolnik, Simona,Stanovnik, Branko
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p. 177 - 189
(2007/10/03)
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